1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  2. Histamine Receptor Cytochrome P450 Potassium Channel
  3. Antihistamine-1

Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.

For research use only. We do not sell to patients.

Antihistamine-1 Chemical Structure

Antihistamine-1 Chemical Structure

CAS No. : 1186430-60-3

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.

IC50 & Target

H1 Receptor

 

CYP2D6

5.4 μM (IC50)

In Vitro

Antihistamine-1 (Compound 2) is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

389.47

Formula

C23H24FN5

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=CN(C2CCN(C3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)N=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (64.19 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5676 mL 12.8380 mL 25.6759 mL
5 mM 0.5135 mL 2.5676 mL 5.1352 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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V2

In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5676 mL 12.8380 mL 25.6759 mL 64.1898 mL
5 mM 0.5135 mL 2.5676 mL 5.1352 mL 12.8380 mL
10 mM 0.2568 mL 1.2838 mL 2.5676 mL 6.4190 mL
15 mM 0.1712 mL 0.8559 mL 1.7117 mL 4.2793 mL
20 mM 0.1284 mL 0.6419 mL 1.2838 mL 3.2095 mL
25 mM 0.1027 mL 0.5135 mL 1.0270 mL 2.5676 mL
30 mM 0.0856 mL 0.4279 mL 0.8559 mL 2.1397 mL
40 mM 0.0642 mL 0.3209 mL 0.6419 mL 1.6047 mL
50 mM 0.0514 mL 0.2568 mL 0.5135 mL 1.2838 mL
60 mM 0.0428 mL 0.2140 mL 0.4279 mL 1.0698 mL
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Antihistamine-1
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HY-100238
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